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PE20020975A1 - DERIVATIVES OF CYCLOPROPYLINDOL AS SELECTIVE INHIBITORS OF SEROTONIN RECAPTATION - Google Patents

DERIVATIVES OF CYCLOPROPYLINDOL AS SELECTIVE INHIBITORS OF SEROTONIN RECAPTATION

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Publication number
PE20020975A1
PE20020975A1 PE2002000243A PE2002000243A PE20020975A1 PE 20020975 A1 PE20020975 A1 PE 20020975A1 PE 2002000243 A PE2002000243 A PE 2002000243A PE 2002000243 A PE2002000243 A PE 2002000243A PE 20020975 A1 PE20020975 A1 PE 20020975A1
Authority
PE
Peru
Prior art keywords
alkyl
alkylene
cyclopropylindol
recaptation
serotonin
Prior art date
Application number
PE2002000243A
Other languages
Spanish (es)
Inventor
Ronald J Mattson
Jonathan L Ditta
John D Catt
Derek J Denhart
Lawrence R Marcin
Dalton King
Jeffrey A Deskus
James R Epperson
Mendi A Higgins
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20020975A1 publication Critical patent/PE20020975A1/en

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    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
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Abstract

SE REFIERE A DERIVADOS DE CICLOPROPILINDOL DE FORMULA I, DONDE A1 ES ALQUILENO C1-C4, ENLACE; A3 ES ALQUILENO C1-C4, ALQUILIDENO C1-C4; A4 ES ALQUILENO C1-C4, ENLACE UNIDO A X, X1, X2; X, X1, X2, X3 SON C, CH; J ES ALQUILO C1-C4; p ES 0-1; R1 Y R2 SON H, ALQUILO C1-C3, CICLOALQUILO C3-C6, FENILO, O-FENILO, ENTRE OTROS; R3 ES H, ALQUILO C1-C4; m ES 0-1; R4 Y R5 SON H, CIANO, HALO, NITRO, PERFLUOROALQUILO C1-C3, O PUEDEN ESTAR UNIDOS A X, X1, X2, X3; n ES 0-1; G ES N, O, S; G1 ES N, CH; Y ES DH; D ES C; Z ES EH; E ES C. SI G ES O, S; m ES CERO; SI G ES N, m ES 1; SI R1 ES NHCOO-ALQUILO C1-C4, ALQUIL C1-C4-NH-COO, ENTRE OTRAS CONDICIONES SON COMPUESTOS PREFERIDOS TRANS-2-[5-CIANOINDOL-3-IL]-1-(N,N-DIMETILAMINOMETIL)CICLOPROPANO; TRANS-(N,N-DIMETILAMINOMETIL)-2-[5-FLUOROINDOL-3-IL]CICLOPROPANO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION DEL COMPUESTO Y DE LOS COMPUESTOS INTERMEDIOS. LOS COMPUESTOS SON INHIBIDORES SELECTIVOS DE LA RECAPTACION DE SEROTONINA Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE DEPRESION, DESORDENES DE ANSIEDAD, EYACULACION PREMATURA, INCONTINENCIA URINARIA, DOLOR CRONICO, DESORDEN OBSESIVO COMPULSIVO, DESORDENES DE LA ALIMENTACIONREFERS TO CYCLOPROPYLINDOL DERIVATIVES OF FORMULA I, WHERE A1 IS C1-C4 ALKYLENE, LINK; A3 IS C1-C4 ALKYLENE, C1-C4 ALKYLIDENE; A4 IS C1-C4 ALKYLENE, X, X1, X2 LINKED; X, X1, X2, X3 ARE C, CH; J IS C1-C4 ALKYL; p IS 0-1; R1 AND R2 ARE H, C1-C3 ALKYL, C3-C6 CYCLOALKYL, PHENYL, O-PHENYL, AMONG OTHERS; R3 IS H, C1-C4 ALKYL; m IS 0-1; R4 AND R5 ARE H, CYANE, HALO, NITRO, C1-C3 PERFLUOROALKYL, OR THEY MAY BE BOUND TO X, X1, X2, X3; n IS 0-1; G IS N, O, S; G1 IS N, CH; Y IS DH; D IS C; Z IS EH; E IS C. IF G IS O, S; m IS ZERO; IF G IS N, m IS 1; IF R1 IS NHCOO-C1-C4 ALKYL, C1-C4 ALKYL-NH-COO, AMONG OTHER CONDITIONS ARE PREFERRED COMPOUNDS TRANS-2- [5-CYANOINDOL-3-IL] -1- (N, N-DIMETHYLAMINOMETHYL) CYCLOPROPANE; TRANS- (N, N-DIMETHYLAMINOMETHYL) -2- [5-FLUOROINDOL-3-IL] CYCLOPROPANE, AMONG OTHERS. IT ALSO REFERS TO A PROCEDURE FOR THE PREPARATION OF THE COMPOUND AND INTERMEDIATE COMPOUNDS. THE COMPOUNDS ARE SELECTIVE INHIBITORS OF SEROTONIN RECAPTATION AND MAY BE USEFUL FOR THE TREATMENT OF DEPRESSION, ANXIETY DISORDERS, PREMATURE EJACULATION, URINARY INCONTINENCE, CHRONIC PAIN, OBSESSIVE COMPULSIVE DISORDER, COMPULSIVE DISORDER

PE2002000243A 2001-03-29 2002-03-27 DERIVATIVES OF CYCLOPROPYLINDOL AS SELECTIVE INHIBITORS OF SEROTONIN RECAPTATION PE20020975A1 (en)

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US27988801P 2001-03-29 2001-03-29
US29312201P 2001-05-23 2001-05-23
US32780401P 2001-10-09 2001-10-09

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PE20020975A1 true PE20020975A1 (en) 2002-10-30

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US (2) US6777437B2 (en)
EP (1) EP1373203A1 (en)
JP (1) JP2004531506A (en)
AR (1) AR035793A1 (en)
BG (1) BG108207A (en)
CA (1) CA2442525A1 (en)
CZ (1) CZ20032644A3 (en)
EE (1) EE200300478A (en)
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